A kind of polypeptide PET imaging agent targeting EGFR and its preparation method and application

A technology of PET imaging agent and polypeptide, which is applied in the field of EGFR-targeting polypeptide PET imaging agent and its preparation and application, can solve the problems of difficult to meet clinical treatment, large side effects of chemotherapy, poor specificity, etc., and achieve good clinical results. Application and development prospects, strong water solubility and good stability

Active Publication Date: 2021-08-31
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For non-solid tumors and cancers with widespread systemic metastases, effective surgical treatment and radiotherapy cannot be performed, and chemotherapy has large side effects, poor specificity, and low curative effect, and it is difficult to meet the needs of clinical treatment.

Method used

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  • A kind of polypeptide PET imaging agent targeting EGFR and its preparation method and application
  • A kind of polypeptide PET imaging agent targeting EGFR and its preparation method and application
  • A kind of polypeptide PET imaging agent targeting EGFR and its preparation method and application

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preparation example Construction

[0030] The preparation method of the polypeptide PET developer of the above target EGFR includes the following steps:

[0031] 1) Apply a cyclotron to bombard 18 O water production 18 F, will then 18 F is conducted to the anion exchange column, then use the column 18 F is washed into the reaction bottle and the azeotropic water is carried out, then 2-bromopropionate and solvent, which is fully reacted, resulting in 2- 18 Ethyl f-propionate;

[0032] 2) 2- 18 F-propionate for alkaline hydrolysis, remove the reaction solvent, mix the hydrolyzate, bis (4-nitrophenyl) ester and solvent, sufficiently react, and then separate semi-prepared HPLC separation purification, obtained 18 F-NFP;

[0033] 3) 18F-NFP, LYS-GE11 polypeptide, N, N-diisopropylamine and solvent mix, adequately reacted, add water to the Sep-Par C-18 column, rinse C-18 column with water, then use ethanol C-18 column, collecting a column, a polypeptide PET developer targeting EGFR ( 18 F-fp-Lys-ge11).

[0034] Preferably...

Embodiment 1

[0048] A method of preparing polypeptides PET imaging agents targeting EGFR comprising the steps of:

[0049] 1) Application of a medical cyclotron bombardment 18 O water, by 18 O (p n) 18 F nuclear reaction production 18 F, will then 18 F-conducting anion exchange column, and the activity was measured using 1mL eluent (12mg of a 4,7,13,16,21,24-hexaoxa-1,10-diazabicyclo [8.8.8] hexacosa alkoxy of K + 3mg 2 CO 3 + 0.15mL + 1.35mL aqueous acetonitrile) to 18 F was rinsed into the reaction flask, blown continuously added to the reaction flask and heated to 110 Helium deg.] C for azeotropic removal of water, drying, adding 5mg of ethyl 2-bromopropionate and 1mL of acetonitrile, 100 ℃ for 10min, to give 2- 18 Ethyl f-propionate;

[0050] 2) in 2 18 Propanoate was added 0.5mL F- concentration of 0.1mol / L potassium hydroxide solution, 100 ℃ hydrolysis 10min, after the reaction solvent was evaporated to dryness, then dissolved hydrolyzate and 40mg 1.5mL carbonate, bis (4-nitro phenyl) ...

Embodiment 2

[0056] A method of preparing polypeptides PET imaging agents targeting EGFR comprising the steps of:

[0057] 1) Application of a medical cyclotron bombardment 18 O water, by 18 O (p n) 18 F nuclear reaction production 18 F, will then 18 F-conducting anion exchange column, and the activity was measured using 1mL eluent (12mg of a 4,7,13,16,21,24-hexaoxa-1,10-diazabicyclo [8.8.8] hexacosa alkoxy of K + 3mg 2 CO 3 + 0.15mL + 1.35mL aqueous acetonitrile) to 18 F was rinsed into the reaction flask, blown continuously added to the reaction flask and heated to 110 Helium deg.] C for azeotropic removal of water, drying, adding 7mg of ethyl 2-bromopropionate and 1mL of acetonitrile, 100 ℃ for 15min, to give 2- 18 Ethyl f-propionate;

[0058] 2) in 2 18 Propanoate was added 0.5mL F- concentration of 0.1mol / L potassium hydroxide solution, 100 ℃ hydrolysis 15min, after the reaction solvent was evaporated to dryness, then dissolved hydrolyzate and 40mg 1.5mL carbonate, bis (4-nitro phenyl) ...

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Abstract

The invention discloses a polypeptide PET imaging agent targeting EGFR, its preparation method and application. The present invention utilizes 18 F‑NFP as a radiochemical labeling intermediate 18 F mark, obtain high-purity PET imaging agent 18 F‑FP‑Lys‑GE11 has good stability, strong water solubility, rapid blood clearance in the body, and is mainly metabolized by the kidneys. The imaging contrast is high, the tumor resolution ability is strong, and it has a good prospect for clinical application and development in tumor PET imaging.

Description

Technical field [0001] The present invention relates to a polypeptide PET developer, which targets EGFR and a preparation method thereof, and applications thereof. Background technique [0002] Malignant tumors are one of the world's largest public health issues, which is extremely harmful to human health. "2017 China Cancer Report" announced the incidence and death data of my country's 2013 cancer, and the report shows that China is a cancer country, and the number of cancer patients accounts for about 40% of the total number of cancer patients. There are about 10,000 people a diagnosis of cancer, average There are seven people diagnosed, all cancer, gastric cancer, colorectal cancer, liver cancer, breast cancer, esophageal cancer in all cancer cases, accounting for 65% of all cancer cases. [0003] Traditional cancer treatment methods mainly include surgical treatment, chemotherapy, radiation therapy, and the like. For non-physical tumors, the whole body is widely transferred c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/08A61K101/02
CPCA61K51/08
Inventor 黄顺胡孔珍韩彦江吴湖炳王全师
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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